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532310 c-Myc Inhibitor IV, KJ-Pyr-9 - CAS 581073-80-5 - Calbiochem

KJ-Pyr-9, C-Myci

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(2-(Furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl)benzamide, KJPyr9, Krohnke Pyridine-9

Primary Target: Myc homodimer
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
581073-80-5C₂₂H₁₅N₃O₄

Products

Catalog NumberPackaging Qty/Pack
5.32310.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable, blood-brain barrier permeant, bioavailable trisubstituted pyridine compound that inhibits c-Myc transcriptional activity. Shown to directly bind to both the monomeric c-Myc (Kd = 6.5 nM) and to c-Myc-Max heterodimer (Kd = 13.4 nM) with high affinity and disrupt c-Myc-Max interaction. Displays a very weak affinity towards Max-Max homodimer (Kd > 1 µM). Also interferes with Max homodimerization, albeit to a lesser extent than c-Myc-Max heterodimerization. Shown to inhibit the c-Myc-driven proliferation of NCI-H460, MDA-MB-231, and SUM-159PT and several other cancer cell lines (IC50 = 5-10 µM). Also diminishes the proliferation of Burkitt lymphoma cell lines expressing high levels of c-Myc (IC50 = 2.5 µM). Suppresses the growth of MDA-MB-231 cells in a xenografted nude mice model (10 mg/kg, i.p., q.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532310
Brand Family Calbiochem®
Synonyms4-(2-(Furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl)benzamide, KJPyr9, Krohnke Pyridine-9
References
ReferencesHart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.
Product Information
CAS number581073-80-5
FormBrown powder
Hill FormulaC₂₂H₁₅N₃O₄
Chemical formulaC₂₂H₁₅N₃O₄
Quality LevelMQ100
Applications
Biological Information
Primary TargetMyc homodimer
Secondary targetMyc-Max
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.32310.0001 04055977287202

Documentation

c-Myc Inhibitor IV, KJ-Pyr-9 - CAS 581073-80-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Hart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-January-2015 JSW
Synonyms4-(2-(Furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl)benzamide, KJPyr9, Krohnke Pyridine-9
DescriptionA cell-permeable, trisubstituted pyridine compound that displays Myc-selective affinity (Kd = 6.5 nM/Myc homodimer, 13.4 nM/Myc-Max dimer, >1.0 µM/Max homodimer) and is 4-times more potent against Myc-Max than Max-Max in DNA-binding assays. Effectively prevents focal microtumors formation following N-Myc, c-Myc, as well as ATG- or CAG-c-Myc transformation of cultured chick embryo fibroblasts/CEF (>99.9% inhibition at 10 µM in ATG-c-Myc-transformed cultures), while exhibiting much reduced or little potency against cultures transformed by v-Src (no inhibition up to 20 µM), v-Jun or PI 3-K H1047R (45.5% inhibition at 10 µM). Selectively inhibits Myc-dependent proliferation of human & avian cultures (Effective conc. 25 to 50 µM; IC50 1 to 10 µM), while exhibiting little potency against Myc-independent growths of human skin fibroblasts, non-transformed, v-jun-transformed, or methylcholanthrene-transformed quail embryo fibroblasts even at a high concentration of 50 µM. Reported to suppress MDA-MB-231-derived tumor expansion in mice (10 mg/kg/d i.p.) in vivo with a concomitant upregulation of N-Myc downregulated gene 1/NDRG1 protein level in tumor tissue. Pharmacokinetics studies reveal good blood-brain barrier permeability in mice ([Drug] = 3.5 µM/plasma & 12.4 µM/brain 4 h post single 10 mg/kg i.p. dosage) and a plasma half-life of 1.84 h in rats following a single i.v. dose of 1 mg/kg.
FormBrown powder
Intert gas (Yes/No) Packaged under inert gas
CAS number581073-80-5
Chemical formulaC₂₂H₁₅N₃O₄
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesHart, J.R., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 12556.